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Flupirtine is a non-opioid analgesic without antipyretic or antiphlogistic properties. Flupirtine is a centrally acting analgesic but the analgesic action of flupirtine does not depend on any central opioid effect. The fact behind this statement is that the pain-relieving property of flupirtine is not reduced by the opioid antagonistic drug naloxone. Flupirtine has been reported for its neuro-protective properties and possess a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Flupertine is transformed into two primary derivatives, 4-fluoro-hippuric acid and the Nacetylated analogue D13223. Both derivatives of are flupirtine pharmacologically active with 30% of the analgesic potency of the parent drug and further oxidized and then conjugated with glycine to form inactive metabolites, Recently, Flupirtine maleate has been introduced in Indian market in oral, intravenous and rectal dosage forms. The half life of flupirtine following intravenous administration was 1.8 hours, while the plasma elimination half life in healthy young volunteers following single dose administration of flupirtine by the intravenous, oral and rectal routes was 8.5, 9.6 and 10.7 hours respectively. There is plenty of literature available on the effect of Flupirtine maleate on chronic and acute pain management. These preliminary finding require confirmation in further comparative studies. [ABSTRACT FROM AUTHOR]

Flupirtine is an amino pyridine derivative that functions as a centrally acting non-opioid, non-steroidal analgesic. It is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Its muscle relaxant properties make it popular for back pain and other orthopedics uses. In the present investigation, recently developed mixed hydrotropic solid dispersion technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. Mixed-hydrotropic solubilisation technique is the experience to increase the solubility of poorly water soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. The Flupirtine loaded solid dispersion was prepared by a solvent evaporation technique using sodium benzoate and a niacinamide hydrotropic mixture. The prepared solid dispersions were valuated regarding their solubility, mean particle size, in-vitro drug release. The prepared solid dispersions were found very stable (chemically). The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability. [ABSTRACT FROM AUTHOR]